Avatrombopag

SKU: orb1220399

Description

Avatrombopag is a new oral thrombopoietin (TPO) receptor agonist activating TPO receptor and increasing megakaryocytic proliferation/differentiation and platelet production.(In Vitro):Avatrombopag (E5501; AKR-501) specifically targets the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as recombinant human TPO (rhTPO) did.Avatrombopag (0-100 nM) supports the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion. Avatrombopag (0-3 μM) induces tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells, as didrhTPO.Avatrombopag promotes megakaryocyte colony formation from human CB CD34+ cells in a concentration-dependent fashion. The EC50 is 25 nM for Avatrombopag and the maximum activity of Avatrombopag is similar to that of rhTPO.(In Vivo):Avatrombopag (0.3-3 mg/kg; p.o.; daily for 14 days) increases the number of human platelets in NOD/SCID mice transplanted with human FL CD34+ cells.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 570406-98-3
• MW: 649.65
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₄Cl₂N₆O₃S₂
• SMILES: O=C(Nc1nc(-c2cc(Cl)cs2)c(N2CCN(C3CCCCC3)CC2)s1)c1cnc(N2CCC(C(=O)O)CC2)c(Cl)c1
• Target: TPO
• Solubility: DMSO:32 mg/mL (49.26 mM)

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AKR-501 | E5501 | YM477

Quick Database Links

Gene Symbol

TPO